Method for making β-secretase co-crystals complexed with a ligand
    1.
    发明授权
    Method for making β-secretase co-crystals complexed with a ligand 有权
    制备与配体络合的β-分泌酶共晶体的方法

    公开(公告)号:US07569391B2

    公开(公告)日:2009-08-04

    申请号:US11634737

    申请日:2006-12-06

    IPC分类号: G01N31/00 G01N33/00

    CPC分类号: C12N9/6421 C07K2299/00

    摘要: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of β-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding human BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

    摘要翻译: 本申请涉及用于生长未络合和复合形式的β-分泌酶(BACE)多肽的晶体的方法。 本申请还涉及未结合的BACE的晶体形式和由晶体确定的BACE的三维结构。 此外,本申请涉及BACE的结晶形式用于鉴定与BACE结合并优选抑制BACE的酶活性的配体,优选抑制剂(拮抗剂)。 此外,本申请涉及编码人BACE多肽的核酸序列和与以前的方法相比制备BACE的方法,导致更有效的结晶。

    REFOLDED RECOMBINANT ALPHA SECRETASE CRYSTALS AND METHODS FOR PREPARING AND USING THE SAME
    2.
    发明申请
    REFOLDED RECOMBINANT ALPHA SECRETASE CRYSTALS AND METHODS FOR PREPARING AND USING THE SAME 有权
    重建的重组ALPHA分泌物晶体及其制备和使用方法

    公开(公告)号:US20100203616A1

    公开(公告)日:2010-08-12

    申请号:US12434897

    申请日:2009-05-04

    IPC分类号: C12N9/50

    CPC分类号: C12N9/6421 C07K2299/00

    摘要: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of β-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

    摘要翻译: 本申请涉及用于生长未络合和复合形式的分泌型(BACE)多肽的晶体的方法。 本申请还涉及未结合的BACE的晶体形式和由晶体确定的BACE的三维结构。 此外,本申请涉及BACE的结晶形式用于鉴定与BACE结合并优选抑制BACE的酶活性的配体,优选抑制剂(拮抗剂)。 此外,本申请涉及编码BACE多肽的核酸序列和与以前的方法相比制备BACE的方法,导致更有效的结晶。

    Refolded recombinant β-secretase crystals and methods for preparing and using the same
    3.
    发明授权
    Refolded recombinant β-secretase crystals and methods for preparing and using the same 有权
    重折叠重组和分泌酶晶体及其制备和使用方法

    公开(公告)号:US08063185B2

    公开(公告)日:2011-11-22

    申请号:US12434897

    申请日:2009-05-04

    IPC分类号: C12N1/12

    CPC分类号: C12N9/6421 C07K2299/00

    摘要: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of β-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

    摘要翻译: 本申请涉及用于生长未络合和复合形式的分泌型(BACE)多肽的晶体的方法。 本申请还涉及未结合的BACE的晶体形式和由晶体确定的BACE的三维结构。 此外,本申请涉及BACE的结晶形式用于鉴定与BACE结合并优选抑制BACE的酶活性的配体,优选抑制剂(拮抗剂)。 此外,本申请涉及编码BACE多肽的核酸序列和与以前的方法相比制备BACE的方法,导致更有效的结晶。

    Codon-optimized β-secretase and methods of refolding and processing
    4.
    发明授权
    Codon-optimized β-secretase and methods of refolding and processing 有权
    密码子优化的β-分泌酶和重折叠和加工的方法

    公开(公告)号:US07166454B1

    公开(公告)日:2007-01-23

    申请号:US10443949

    申请日:2003-05-22

    CPC分类号: C12N9/6421 C07K2299/00

    摘要: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of β-secretase (BACE) polypeptide. Polypeptides used herein are derived from human BACE which is also known by the synonyms “mamapsin 2”, “human β-site APP-cleaving enzyme, and Asp2”. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

    摘要翻译: 本申请涉及用于生长未络合和复合形式的β-分泌酶(BACE)多肽的晶体的方法。 本文使用的多肽衍生自人BACE,其同义词“mamapsin 2”,“human beta-site APP-cleaving enzyme,and Asp2”也是已知的。 本申请还涉及未结合的BACE的晶体形式和由晶体确定的BACE的三维结构。 此外,本申请涉及BACE的结晶形式用于鉴定与BACE结合并优选抑制BACE的酶活性的配体,优选抑制剂(拮抗剂)。 此外,本申请涉及编码BACE多肽的核酸序列和与以前的方法相比制备BACE的方法,导致更有效的结晶。